{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,3]],"date-time":"2026-10-03T03:46:32Z","timestamp":1790999192510,"version":"4.1.0"},"reference-count":23,"publisher":"Wiley","issue":"5","license":[{"start":{"date-parts":[[2020,1,9]],"date-time":"2020-01-09T00:00:00Z","timestamp":1578528000000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/creativecommons.org\/licenses\/by-nc-nd\/4.0\/"}],"content-domain":{"domain":["chemistry-europe.onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["ChemMedChem"],"published-print":{"date-parts":[[2020,3,5]]},"abstract":"<jats:title>Abstract<\/jats:title><jats:p>There is an urgent clinical need for imaging of \u03b1\u2010synuclein (\u03b1Syn) fibrils, the hallmark biomarker for Parkinson's disease, in neurodegenerative disorders. Despite immense efforts, promising tracer candidates for nuclear imaging of \u03b1Syn are rare. Diphenyl pyrazoles are known modulators of \u03b1Syn aggregation and thus bear potential for non\u2010invasive detection of this biomarker in\u2005vivo. Here we demonstrate high\u2010affinity binding of the family member anle253b to fibrillar \u03b1Syn and present a high\u2010yielding site\u2010selective radiosynthesis route for <jats:sup>11<\/jats:sup>C radiolabeling using in\u2010situ generated [<jats:sup>11<\/jats:sup>C]formaldehyde and reductive methylation. Radio\u2010HPLC of the tracer after incubation with rat serum in\u2005vitro shows excellent stability of the molecule. Positron emission tomography in healthy animals is used to assess the pharmacokinetics and biodistribution of the tracer, showing good penetration of the blood\u2013brain barrier and low background binding to the non\u2010pathological brain.<\/jats:p>","DOI":"10.1002\/cmdc.201900689","type":"journal-article","created":{"date-parts":[[2019,12,20]],"date-time":"2019-12-20T07:39:57Z","timestamp":1576827597000},"page":"411-415","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":51,"title":["<sup>11<\/sup>C Radiolabeling of anle253b: a Putative PET Tracer for Parkinson's Disease That Binds to \u03b1\u2010Synuclein Fibrils in\u2005vitro and Crosses the Blood\u2010Brain Barrier"],"prefix":"10.1002","volume":"15","author":[{"ORCID":"https:\/\/orcid.org\/0000-0003-2412-5361","authenticated-orcid":false,"given":"Andreas","family":"Maurer","sequence":"first","affiliation":[{"name":"Werner Siemens Imaging Center, Department of Preclinical 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